Local Anesthetic Hydrogel Composition for Sustained Release
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Solution Overview
Problem
Current local anesthetic compositions provide short-lived pain relief, necessitating continuous infusion and systemic opioids, which have adverse side effects, and existing long-acting alternatives are not effective.
Innovation Solution
A pharmaceutical composition comprising a gel polymer matrix of methylcellulose and hyaluronan with a local anesthetic agent, designed for sustained release, which includes a dosage form of 0.1-3.0% methylcellulose and 1.0-2.0% methylcellulose and 1.0 to 3.0 wt% hyaluronan in the form of a gel polymer matrix, and at least one local anesthetic agent, which includes a dosage form of 0.1-3.0 wt% methylcellulose and 0.1-3.0 wt% hyaluronan, with a local anesthetic agent, providing a sustained release profile.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Speed
If local anesthetic is administered in solution form, then rapid onset of action is achieved, but duration of action is short
Solution Approach 1:
The anesthetic is segmented into two forms: dissolved anesthetic (acid addition salt) for rapid onset and suspended free-base particles for sustained release. This segmentation allows the composition to provide both rapid initial effect and prolonged duration without requiring continuous infusion.
Solution Approach 2:
The invention changes the physical and chemical parameters of the anesthetic by using both acidic and basic forms with specific ratios. The acidic form (salt) provides water solubility for rapid absorption, while the basic form (free-base particles) provides sustained release, thereby resolving the contradiction between rapid onset and prolonged duration.
2Duration of action of moving object
If local anesthetic is administered continuously to maintain effect, then duration of action is extended, but systemic opioid use increases with adverse side effects
Solution Approach 1:
The composition provides continuous local anesthetic action through the sustained release of free-base particles over time. This continuous local effect eliminates the need for repeated administrations or systemic opioid supplementation, thereby extending duration of action while avoiding the harmful effects of continuous infusion and systemic opioids.
Solution Approach 2:
The gel polymer matrix acts as an intermediary carrier that controls the release of the anesthetic. It maintains the anesthetic at the site of administration, providing prolonged local effect without requiring systemic circulation or continuous external infusion, thus avoiding systemic side effects.
3Quantity of substance
If high concentration of local anesthetic is used, then potency is increased, but risk of toxicity increases
Solution Approach 1:
The composition dynamically releases the anesthetic over time rather than providing a static high concentration. The free-base particles gradually dissolve and release anesthetic, maintaining therapeutic levels while avoiding peak toxic concentrations. This dynamic release profile allows use of higher total anesthetic quantities without increasing immediate toxicity risk.
Solution Approach 2:
The anesthetic is pre-formulated in a controlled release composition with specific ratios of acidic and basic forms. This preliminary preparation ensures that the anesthetic is released in a controlled manner, preventing sudden high concentrations that could cause toxicity while still providing sufficient total dose for effective pain relief.
4Ease of operation
If single injection is used, then ease of administration is improved, but duration of action is insufficient
Solution Approach 1:
The invention uses a composite formulation containing both dissolved anesthetic (acid addition salt) and suspended anesthetic (free-base particles) in a gel polymer matrix. This composite structure allows a single injection to provide both rapid onset and prolonged duration, eliminating the need for multiple injections or continuous infusion while maintaining ease of administration.
Applied Scientific Principles
This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.
Function Achieved in This Case
The composition achieves prolonged local anesthetic effects for at least 12 hours to 7 days, reducing the need for continuous infusion and systemic opioids, while maintaining a safe and effective anesthetic concentration.
Implementation Method 1
sustained release local anesthetic hydrogel composition
Implementation Method 2
pharmaceutical composition comprising: 1.8 wt% to 3 wt% methylcellulose and 0.1 wt% to 3 wt% hyaluronan in the form of a gel polymer matrix
Data Source
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AI summary
A bioresorbable, sustained release pharmaceutical composition comprising: 1.8 wt% to 3.0 wt% methylcellulose and 0.1 wt% to 3.0 wt% hyaluronan in the form of a gel polymer matrix, and at least one local anesthetic agent, suitably ropivacaine, which may be administered by injection.